Postoperative AnalgesiaPhase 1NCT07717086
Pharmacokinetic and Safety Study of HYR-PB21 vs Bupivacaine Hydrochloric Acid in Healthy Participants
A Phase 1 study testing HYR-PB21， 100 mg, HYR-PB21， 200 mg and HYR-PB21， 400 mg in people with Postoperative Analgesia, run by Fruithy Holdings Limited.
Trial summary
This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study to evaluate the safety and pharmacokinetic (PK) profile of HYR-PB21, a pamoate-formulated bupivacaine injectable, in healthy adult participants. Read more about this study
- Who is it for?
- Ages 18 to 50 yearsHealthy volunteers can take part
- Conditions the study is for
- Postoperative Analgesia
- What is being tested?
- HYR-PB21， 100 mg, HYR-PB21， 200 mg and HYR-PB21， 400 mg
- Type of treatment
- Injection or infusion
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 28 participants
- Where
- No sites listed yet
- Study dates
- Aug 2026to Oct 2026
- Phase
- Phase 1
- Are there results?
- Not yet: the study is under way
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 50 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy male or female adult participants
- Age 18 to 50 years old (inclusive)
- Body mass index (BMI) of 18.0 to 32.0 kg/m2 and weight ≥50 kg.
- Participant is generally healthy, as determined by the Investigator based on medical history, physical examination, clinical laboratory test results, vital signs, and 12-lead electrocardiogram (ECG) at screening.
- Additional Detailed Inclusion Criteria Include:
- Female participants who engage in heterosexual intercourse must be non-pregnant or non-lactating. Female participants of childbearing potential must agree to use 2 acceptable methods of contraception with their male partner from screening until 6 months after the last dose of the study drug and refrain from donating ovum for this same period. (Refer to contraception section).Females of non-childbearing potential must either be :
Show all 17Show fewer
- Post menopausal as defined by at least 12 months of consecutive Amenorrhea and Follicle-Stimulating Hormone(FSH) and estradiol confirming Post menopausal status at screening. See Appendix Section 13 for additional details.
- Surgically sterile at least 6 months prior to screening with documentation.
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- Bilateral tubal ligation
- Hysterectomy (partial or total)
- Bilateral salpingectomy
- Bilateral oophorectomy
- Male participants, if sexually active with a female partner of child-bearing potential, must be vasectomized or agree to take appropriate precautions to prevent conception, including practicing an effective method of contraception, and must not donate sperm from screening through 12 weeks following administration of the last dose of study medication.
- Only non-smokers are eligible. For a period of at least six months prior to Screening, all participants must have been free from excessive alcohol intake or regular use of illegal recreational drugs. Participants with any past or current history of marijuana use are not eligible for the study.
- Ability to understand and willingness to sign a written informed consent form (The consent form must be signed by the participant prior to any study-specific procedures.)
- Willingness and able to comply with catheter placement and blood draws throughout the course of study and comply with study procedures and follow-up examination.
Who cannot join
- Participants will be excluded if they have
- A history of hypersensitivity or idiosyncratic reactions to amide-type local anesthetics;
- Have a personal or family history of clotting disorder or hematologic abnormality, such as excessive bleeding, joint hematoma, thrombovascular disease, thrombocytopenia, or any chronic condition requiring treatment with transfusions; have a history of recurrent bleeding episodes (eg, epistaxis, bruising or gingival bleeding) within 1 month prior to Screening, or a longstanding history of such bleeding.
- Participants who were detected to have Glucose-6-phosphate dehydrogenase(G6PD) deficiency during the screening period.
- Additional detailed exclusion criteria include:
- Females who are pregnant, lactating, or have plans to become pregnant during the study
Show all 37Show fewer
- History and/or recent evidence within six months prior to Screening of alcohol or drug/substance abuse disorder
- History of clinically significant allergies, including drug allergies, or allergic bronchial asthma, or related bronchospastic conditions
- Participants who have a history of unexplained syncope or fainting or a condition that predisposes them to syncope, such as hypotension, orthostatic hypotension, bradycardia, or dehydration.
- Participants who have used P-gp and/or Cytochrome P450 hepatic microsomal enzyme-inducing or inhibiting drugs (e.g., propafenone, voriconazole, fluconazole, cimetidine) within 30 days of first dosing, refer to Appendix 15-16 for detailed list
- Participants with a history or presence of significant cardiovascular, pulmonary, hepatic, gallbladder or biliary tract, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, psychiatric disease, or active sexually transmitted disease to include:
- Current or history of thrombosis or thromboembolic disorders
- Any history of malignancy, especially breast cancer or other hormone-sensitive cancers
- Undiagnosed abnormal vaginal bleeding unrelated to pregnancy
- Cholestatic jaundice of pregnancy
- Liver tumors, benign or malignant, or active liver disease
- Uncontrolled hypertension
- History or evidence of acute or chronic respiratory disorders, including but not limited to chronic obstructive pulmonary disease (COPD) or asthma
- History or presence of significant cardiovascular abnormalities, including, without limitation, severe bradycardia, sick sinus syndrome, second- or third-degree atrial ventricular block, long QT syndrome, cardiogenic shock, and decompensated heart failure
- Participant family history of sudden cardiac death or long QT syndrome and baseline QT prolongation >450 for males and >470 for females at screening
- Participants with estimated glomerular filtration rate (eGFR - utilizing Chronic Kidney Disease Epidemiology Collaboration formula) < 80 mL/min/1.73 m2; participants with slightly lower values may be included upon agreement between the sponsor medical representative and the Principal Investigator at screening
- Participants meeting any of the following laboratory criteria will be excluded:
- Screening total bilirubin > 1.3 mg/dL; participants with a documented history of Gilbert's syndrome can be enrolled if the direct bilirubin is < 0.4 mg/dL
- Screening alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) > upper limits of normal (ULN)
- Screening platelets < 140,000/microliter
- Screening international normalized ratio > 1.2
- Participants who test positive at screening for human immunodeficiency virus (HIV), Hepatitis B surface antigen (HBsAg), or Hepatitis C virus (HCV) antibody
- Participants who test positive at Screening and/or admission (Day 0) for alcohol and/or drugs of abuse
- Participants who donated ≥ 500 mL of blood within 56 days prior to the study period or ≥ 50 mL and ≤ 499 mL of blood within 30 days prior to the study period
- Participants who are unable to refrain from or anticipatethe use of any medication, including prescription and non-prescription drugs or herbal remedies (such as St. John's Wort [Hypericum perforatum]) approximately 2 weeks prior to study drug administration.
- Participant who is unable to refrain from excessive alcohol consumption within one week prior to the study start throughout the study, until the final study visit. Moderate alcohol consumption is defined as one standard drink per day for women and two drinks per day for men; whereby one standard drink is equivalent to 12 oz beer (5% alcohol), 5 ounces of wine (12% alcohol), and 1.5 ounces of 80 proof (40% alcohol). Excessive consumption would be considered consistently in excess of twice the moderate recommendation.
- Participant who consumes excessive amounts of caffeine for one month prior to the study drug administration, defined as greater than six servings (one serving is approximately equivalent to 120 mg of caffeine) of coffee, tea, cola, or other caffeinated beverages per day
- Participants who donated plasma (e.g., plasmapheresis) within 14 days prior to the study period; participants will be advised not to donate plasma for 14 days after completing the study
- Participant with tattoos to the abdominal area, which in the opinion of the investigator, could interfere with study drug administration.
- Participant has poor venous access or has a history of difficulty tolerating venipuncture such as vasovagal syncope.
- Participants who have participated in another clinical trial which required blood draws within 30 days prior to the first study drug dosing
- Have any other condition that, in the opinion of the Investigator, would interfere with a participant's ability to adhere to the protocol, interfere with assessment of the investigational product, or compromise the safety of the participant or the quality of the data.
Trial locations and contacts
No sites are listed yet. Contact the study team or a site near you to ask about taking part.
About this study
Official title: A Phase I, Randomized, Single-blind, Active-controlled, Parallel Study to Evaluate the Safety and Pharmacokinetics of Single-Dose HYR-PB21 Versus Bupivacaine Hydrochloric Acid for Subcutaneous Injection in Healthy Participants
This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study to evaluate the safety and pharmacokinetic (PK) profile of HYR-PB21, a pamoate-formulated bupivacaine injectable, in healthy adult participants.
Participants are randomized to receive a single subcutaneous dose of HYR-PB21 at one of three dose levels (100 mg, 200 mg, or 400 mg) or a single 100 mg dose of Bupivacaine hydrochloride injection (as base) as active control.
The primary objectives are to characterize the PK profile of HYR-PB21 at the three dose levels compared with Bupivacaine hydrochloride, and to determine the Pharmacokinetics characteristics of the pamoic acid moiety following HYR-PB21 administration. Secondary objectives are to extend cumulative safety and tolerability observations of single subcutaneous doses of HYR-PB21 in healthy adults.
Read the detailed description
Background and Rationale
HYR-PB21 for Injectable Suspension (HYR-PB21) is a novel long-acting formulation under investigation for local analgesia. Preclinical and clinical data supporting this investigational new drug include four previous Phase 1 or 2 studies conducted in Chinese participants and one Phase 1 study in Australian participants. These prior studies evaluated the pharmacokinetics (PK), pharmacodynamics, safety, and tolerability of HYR-PB21. The current study is designed to serve as a bridging study to extrapolate the existing ex-US PK and safety data to a North American population. Upon successful completion, the data from this study will be utilized to define the proposed Phase 3 efficacy dose or dose range for North American patients.
Study Design and Objectives
This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study designed to evaluate the safety and pharmacokinetic profile of HYR-PB21 compared to Bupivacaine HCl Injection in healthy adult participants.
The primary objectives are:
To characterize and compare the plasma PK profile of three dose levels of HYR-PB21 (100 mg, 200 mg, and 400 mg) versus a single dose of 100 mg Bupivacaine hydrochloride Injection (calculated as base).
To determine the pharmacokinetic characteristics of the pamoic acid component following administration of HYR-PB21 at the aforementioned dose levels.
The secondary objective is to further evaluate the cumulative safety and tolerability of single subcutaneous doses of HYR-PB21 in healthy participants.
Participants and Interventions
A total of 28 healthy adult participants will be randomized in a 1:1:1:1 ratio into four parallel treatment arms (N=7 per arm).All treatments will be administered via subcutaneous injection.
Extensive blood sampling will be conducted to characterize the plasma concentration-time profiles. Sampling time points are: pre-dose (within 2 hours prior to dosing), 15 (±2) min, 30 (±2) min, 1 (±2) h, 2 (±3) h, 4 (±3) h, 8 (±5) h, 12 (±5) h, 18 (±5) h, 24 (±5) h, 30 (±5) h, 36 (±5) h, 48 (±5) h, 60 (±5) h, 72 (±5) h, 96 (±5) h, 120 (±5) h, and 144 (±5) h post-dose.
Safety and tolerability will be monitored throughout the study duration. Assessments include:
Treatment-emergent adverse events (TEAEs), including monitoring for Local Anesthetic Systemic Toxicity (LAST) and local injection site reactions, etc.
- Conditions
- Postoperative Analgesia
- Being tested
- HYR-PB21， 100 mg, HYR-PB21， 200 mg, HYR-PB21， 400 mg, Bupivacaine hydrochloride， 100 mg (as base)
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
HYR-PB21， 100 mgDrug
Also called Bupivacaine Pamoic acid Injection， 100 mg
HYR-PB21， 100 mg, administered as a single subcutaneous injection.
HYR-PB21， 200 mgDrug
Also called Bupivacaine Pamoic acid Injection， 200 mg
HYR-PB21 200 mg, administered as a single subcutaneous injection.
HYR-PB21， 400 mgDrug
Also called Bupivacaine Pamoic acid Injection， 400 mg
HYR-PB21 400 mg, administered as a single subcutaneous injection.
Bupivacaine hydrochloride， 100 mg (as base)Drug
Also called MARCAINE®， 100 mg
Bupivacaine Hydrochloric acid injection 100 mg (expressed as bupivacaine base), administered as a single subcutaneous injection. Active comparator.
| Study group | Role | What they receive |
|---|---|---|
| HYR-PB21， 100 mg | Experimental | HYR-PB21， 100 mg， administered as a single subcutaneous injection Receives: Drug: HYR-PB21， 100 mg |
| HYR-PB21， 200 mg | Experimental | HYR-PB21， 200 mg，administered as a single subcutaneous injection Receives: Drug: HYR-PB21， 200 mg |
| HYR-PB21， 400 mg | Experimental | HYR-PB21， 400 mg， administered as a single subcutaneous injection Receives: Drug: HYR-PB21， 400 mg |
| Bupivacaine hydrochloride， 100 mg (as base) | Active comparator | Bupivacaine hydrochloride， 100 mg， administered as a single subcutaneous injection Receives: Drug: Bupivacaine hydrochloride， 100 mg (as base) |
What is being measured
The primary outcome is the main question the study is designed to answer.
Maximum observed plasma concentration(Cmax) of bupivacaine
The maximum observed plasma concentrations of bupivacaine was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Maximum observed plasma concentration(Cmax) of pamoic acid
The maximum observed plasma concentrations of pamoic acid was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Area Under the Curve(AUC0-t) of bupivacaine
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of bupivacaine was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Area Under the Curve(AUC0-t) of pamoic acid
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of pamoic acid was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Terminal elimination half-life(t1/2) of bupivacaine
The apparent terminal half-life of bupivacaine was calculated using the formula ln(2)/λz, where λz is the terminal elimination rate constant determined through linear regression of the logarithm of the final stage concentration (at least 3 data points, along with the R² value). The unit is hour.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Terminal elimination half-life(t1/2) of pamoic acid
The apparent terminal half-life of pamoic acid was calculated using the formula ln(2)/λz, where λz is the terminal elimination rate constant determined through linear regression of the logarithm of the final stage concentration (at least 3 data points, along with the R² value). The unit is hour.
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Time of maximum observed plasma concentration(Tmax) of bupivacaine
The time at which bupivacaine reach their maximum plasma concentrations is recorded based on the actual sampling time corresponding to the Cmax value (if there are multiple identical Cmax values, the time of the first occurrence is taken as the reference). Unit: hour
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Time of maximum observed plasma concentration(Tmax) of pamoic acid
The time at which pamoic acid reach their maximum plasma concentrations is recorded based on the actual sampling time corresponding to the Cmax value (if there are multiple identical Cmax values, the time of the first occurrence is taken as the reference). Unit: hour
Measured: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
Secondary outcomes (1)
Number of participants with abnormal laboratory tests results, abnormal vital signs,abnormal ECG readings, abnormal physical examination findings
Laboratory tests include hematology (e.g., hemoglobin, white blood cell count, platelet count), blood chemistry (e.g., Alanine Aminotransferase, Aspartate Aminotransferase, total bilirubin, creatinine, glucose), urinalysis, and coagulation (e.g., Prothrombin Time, Activated Partial Thromboplastin Time). Vital signs include sitting systolic/diastolic blood pressure, pulse rate, respiratory rate, and body temperature. Abnormal is defined as a value outside the institutional reference range. Clinically significant abnormal values will also be summarized separately, defined as CTCAE Grade ≥1 . Values are summarized as number (%) of participants.
Measured: Baseline through Day 28 (or 30 days post-dose)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted21 Jul 2026
- Study startAug 2026 (estimated)
- Primary completionSep 2026 (estimated)
- Study completionOct 2026 (estimated)
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Postoperative AnalgesiaStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Parallel groups
- Masking
- Single blind
- Who is masked
- Participant
- Enrolment
- 28 participants (estimated)
Sponsor and investigators
- Lead sponsor
- Fruithy Holdings Limited
- Sponsor type
- Industry (pharma, biotech, devices)
- Collaborators
- Frontage Clinical Services
- Responsible party
- Sponsor
- Investigators
- shanchun zhang, Doctor, Study director, Fruithy Holdings Limited
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT07717086
- Sponsor's protocol ID
- HYR-PB21-US-01
- Status last verified
- Aug 2026
- First submitted
- 10 Jul 2026
- Last updated
- 24 Aug 2026
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
- Individual data sharing
- No
Study at a glance
From the registry record, last updated by the sponsor on 24 Aug 2026. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase I, Randomized, Single-blind, Active-controlled, Parallel Study to Evaluate the Safety and Pharmacokinetics of Single-Dose HYR-PB21 Versus Bupivacaine Hydrochloric Acid for Subcutaneous Injection in Healthy Participants
- ClinicalTrials.gov ID
- NCT07717086
- Acronym / sponsor ID
- HYR-PB21-US-01
- Conditions
- Postoperative Analgesia
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Not yet recruiting
- Enrolment
- 28 participants (estimated)
- Lead sponsor
- Fruithy Holdings LimitedIndustry (pharma, biotech, devices)
- Collaborators
- Frontage Clinical Services
- Study start
- Aug 2026 (estimated)
- Primary completion
- Sep 2026 (estimated)
- Study completion
- Oct 2026 (estimated)
- First posted
- 21 Jul 2026 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study to evaluate the safety and pharmacokinetic (PK) profile of HYR-PB21, a pamoate-formulated bupivacaine injectable, in healthy adult participants.
Participants are randomized to receive a single subcutaneous dose of HYR-PB21 at one of three dose levels (100 mg, 200 mg, or 400 mg) or a single 100 mg dose of Bupivacaine hydrochloride injection (as base) as active control.
The primary objectives are to characterize the PK profile of HYR-PB21 at the three dose levels compared with Bupivacaine hydrochloride, and to determine the Pharmacokinetics characteristics of the pamoic acid moiety following HYR-PB21 administration. Secondary objectives are to extend cumulative safety and tolerability observations of single subcutaneous doses of HYR-PB21 in healthy adults.
Detailed description
Background and Rationale
HYR-PB21 for Injectable Suspension (HYR-PB21) is a novel long-acting formulation under investigation for local analgesia. Preclinical and clinical data supporting this investigational new drug include four previous Phase 1 or 2 studies conducted in Chinese participants and one Phase 1 study in Australian participants. These prior studies evaluated the pharmacokinetics (PK), pharmacodynamics, safety, and tolerability of HYR-PB21. The current study is designed to serve as a bridging study to extrapolate the existing ex-US PK and safety data to a North American population. Upon successful completion, the data from this study will be utilized to define the proposed Phase 3 efficacy dose or dose range for North American patients.
Study Design and Objectives
This is a Phase I, randomized, single-blind, active-controlled, single-dose, parallel-group study designed to evaluate the safety and pharmacokinetic profile of HYR-PB21 compared to Bupivacaine HCl Injection in healthy adult participants.
The primary objectives are:
To characterize and compare the plasma PK profile of three dose levels of HYR-PB21 (100 mg, 200 mg, and 400 mg) versus a single dose of 100 mg Bupivacaine hydrochloride Injection (calculated as base).
To determine the pharmacokinetic characteristics of the pamoic acid component following administration of HYR-PB21 at the aforementioned dose levels.
The secondary objective is to further evaluate the cumulative safety and tolerability of single subcutaneous doses of HYR-PB21 in healthy participants.
Participants and Interventions
A total of 28 healthy adult participants will be randomized in a 1:1:1:1 ratio into four parallel treatment arms (N=7 per arm).All treatments will be administered via subcutaneous injection.
Extensive blood sampling will be conducted to characterize the plasma concentration-time profiles. Sampling time points are: pre-dose (within 2 hours prior to dosing), 15 (±2) min, 30 (±2) min, 1 (±2) h, 2 (±3) h, 4 (±3) h, 8 (±5) h, 12 (±5) h, 18 (±5) h, 24 (±5) h, 30 (±5) h, 36 (±5) h, 48 (±5) h, 60 (±5) h, 72 (±5) h, 96 (±5) h, 120 (±5) h, and 144 (±5) h post-dose.
Safety and tolerability will be monitored throughout the study duration. Assessments include:
Treatment-emergent adverse events (TEAEs), including monitoring for Local Anesthetic Systemic Toxicity (LAST) and local injection site reactions, etc.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Parallel groups
- Masking
- Single blind (participant)
- Number of arms
- 4
| Arm | Type | Receives |
|---|---|---|
| HYR-PB21， 100 mg | Experimental | Drug: HYR-PB21， 100 mgHYR-PB21， 100 mg， administered as a single subcutaneous injection |
| HYR-PB21， 200 mg | Experimental | Drug: HYR-PB21， 200 mgHYR-PB21， 200 mg，administered as a single subcutaneous injection |
| HYR-PB21， 400 mg | Experimental | Drug: HYR-PB21， 400 mgHYR-PB21， 400 mg， administered as a single subcutaneous injection |
| Bupivacaine hydrochloride， 100 mg (as base) | Active comparator | Drug: Bupivacaine hydrochloride， 100 mg (as base)Bupivacaine hydrochloride， 100 mg， administered as a single subcutaneous injection |
Who may qualify
- Ages
- 18 to 50 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (17 listed)
- Healthy male or female adult participants
- Age 18 to 50 years old (inclusive)
- Body mass index (BMI) of 18.0 to 32.0 kg/m2 and weight ≥50 kg.
- Participant is generally healthy, as determined by the Investigator based on medical history, physical examination, clinical laboratory test results, vital signs, and 12-lead electrocardiogram (ECG) at screening.
- Female participants who engage in heterosexual intercourse must be non-pregnant or non-lactating. Female participants of childbearing potential must agree to use 2 acceptable methods of contraception with their male partner from screening until 6 months after the last dose of the study drug and refrain from donating ovum for this same period. (Refer to contraception section).Females of non-childbearing potential must either be :
Key exclusion criteria (37 listed)
- Participants will be excluded if they have
- A history of hypersensitivity or idiosyncratic reactions to amide-type local anesthetics;
- Have a personal or family history of clotting disorder or hematologic abnormality, such as excessive bleeding, joint hematoma, thrombovascular disease, thrombocytopenia, or any chronic condition requiring treatment with transfusions; have a history of recurrent bleeding episodes (eg, epistaxis, bruising or gingival bleeding) within 1 month prior to Screening, or a longstanding history of such bleeding.
- Participants who were detected to have Glucose-6-phosphate dehydrogenase(G6PD) deficiency during the screening period.
- Females who are pregnant, lactating, or have plans to become pregnant during the study
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| HYR-PB21， 100 mgAlso: Bupivacaine Pamoic acid Injection， 100 mgHYR-PB21， 100 mg, administered as a single subcutaneous injection. | Drug | HYR-PB21， 100 mg |
| HYR-PB21， 200 mgAlso: Bupivacaine Pamoic acid Injection， 200 mgHYR-PB21 200 mg, administered as a single subcutaneous injection. | Drug | HYR-PB21， 200 mg |
| HYR-PB21， 400 mgAlso: Bupivacaine Pamoic acid Injection， 400 mgHYR-PB21 400 mg, administered as a single subcutaneous injection. | Drug | HYR-PB21， 400 mg |
| Bupivacaine hydrochloride， 100 mg (as base)Also: MARCAINE®， 100 mgBupivacaine Hydrochloric acid injection 100 mg (expressed as bupivacaine base), administered as a single subcutaneous injection. Active comparator. | Drug | Bupivacaine hydrochloride， 100 mg (as base) |
Primary outcome
Maximum observed plasma concentration(Cmax) of bupivacaine
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The maximum observed plasma concentrations of bupivacaine was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Maximum observed plasma concentration(Cmax) of pamoic acid
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The maximum observed plasma concentrations of pamoic acid was directly obtained from the observed concentration-time curves. Units: ng/mL. The PK parameters will be analyzed using the non-partial model. For ease of statistical comparison, the Cmax values will be log-transformed.
Area Under the Curve(AUC0-t) of bupivacaine
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of bupivacaine was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Area Under the Curve(AUC0-t) of pamoic acid
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
During the period from time zero (the administration time) to Tlast (the last time point when the concentration reaches or exceeds the quantitative lower limit), the area under the plasma concentration-time curve of pamoic acid was calculated according to the mixed logarithmic linear trapezoidal rule. Unit: ng·hour/mL.
Terminal elimination half-life(t1/2) of bupivacaine
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The apparent terminal half-life of bupivacaine was calculated using the formula ln(2)/λz, where λz is the terminal elimination rate constant determined through linear regression of the logarithm of the final stage concentration (at least 3 data points, along with the R² value). The unit is hour.
Terminal elimination half-life(t1/2) of pamoic acid
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The apparent terminal half-life of pamoic acid was calculated using the formula ln(2)/λz, where λz is the terminal elimination rate constant determined through linear regression of the logarithm of the final stage concentration (at least 3 data points, along with the R² value). The unit is hour.
Time of maximum observed plasma concentration(Tmax) of bupivacaine
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The time at which bupivacaine reach their maximum plasma concentrations is recorded based on the actual sampling time corresponding to the Cmax value (if there are multiple identical Cmax values, the time of the first occurrence is taken as the reference). Unit: hour
Time of maximum observed plasma concentration(Tmax) of pamoic acid
Time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose
The time at which pamoic acid reach their maximum plasma concentrations is recorded based on the actual sampling time corresponding to the Cmax value (if there are multiple identical Cmax values, the time of the first occurrence is taken as the reference). Unit: hour
1 secondary outcome
Number of participants with abnormal laboratory tests results, abnormal vital signs,abnormal ECG readings, abnormal physical examination findings
Time frame: Baseline through Day 28 (or 30 days post-dose)
Results and safety
This study is still under way. Results are not available in the source record yet.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 24 Aug 2026.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part.
shanchun zhang, Doctor study director
Fruithy Holdings Limited
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing HYR-PB21， 100 mg, HYR-PB21， 200 mg and HYR-PB21， 400 mg in people with Postoperative Analgesia, run by Fruithy Holdings Limited.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 17 inclusion and 37 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: opening soon, as of the sponsor's last update on 24 Aug 2026. Status can change between updates, so confirm with the study contact before making plans.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
This study is still under way. Results are not available in the source record yet.
How can a doctor refer a patient or contact the research team?
Contact Lisa Mulligan, Bachelor (Mulligan, lmulligan@frontagelab.com), or a site near the patient. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Maximum observed plasma concentration(Cmax) of bupivacaine (time frame: Predose; 0.25, 0.5, 1, 2, 4, 8, 12, 18, 24, 30, 36, 48, 60, 72, 96, 120, 144, 168 hours and Day 14 post-dose). The study lists 8 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 24 Aug 2026.